Department of Medicinal Chemistry, Virginia Commonwealth University, Richmond, Virginia, USA.
Department of Pharmacoinformatics, National Institute of Pharmaceutical Education and Research (NIPER), S.A.S. Nagar, Punjab, India.
Drug Dev Res. 2023 Dec;84(8):1624-1651. doi: 10.1002/ddr.22113. Epub 2023 Sep 11.
Alzheimer's disease (AD) is a progressive age-related neurodegenerative brain disorder, which leads to loss of memory and other cognitive dysfunction. The underlying mechanisms of AD pathogenesis are very complex and still not fully explored. Cholinergic neuronal loss, accumulation of amyloid plaque, metal ions dyshomeostasis, tau hyperphosphorylation, oxidative stress, neuroinflammation, and mitochondrial dysfunction are major hallmarks of AD. The current treatment options for AD are acetylcholinesterase inhibitors (donepezil, rivastigmine, and galantamine) and NMDA receptor antagonists (memantine). These FDA-approved drugs mainly provide symptomatic relief without addressing the pathological aspects of disease progression. So, there is an urgent need for novel drug development that not only addresses the basic mechanisms of the disease but also shows the neuroprotective property. Various research groups across the globe are working on the development of multifunctional agents for AD amelioration using different core scaffolds for their design, and carbamate is among them. Rivastigmine was the first carbamate drug investigated for AD management. The carbamate fragment, a core scaffold of rivastigmine, act as a potential inhibitor of acetylcholinesterase. In this review, we summarize the last 10 years of research conducted on the modification of carbamate with different substituents which primarily target ChE inhibition, reduce oxidative stress, and modulate Aβ aggregation.
阿尔茨海默病(AD)是一种进行性与年龄相关的神经退行性脑疾病,可导致记忆丧失和其他认知功能障碍。AD 发病机制的潜在机制非常复杂,仍未完全探索。胆碱能神经元丧失、淀粉样斑块积累、金属离子动态平衡失调、tau 过度磷酸化、氧化应激、神经炎症和线粒体功能障碍是 AD 的主要标志。目前 AD 的治疗选择是乙酰胆碱酯酶抑制剂(多奈哌齐、利斯的明和加兰他敏)和 NMDA 受体拮抗剂(美金刚)。这些获得 FDA 批准的药物主要提供症状缓解,而不能解决疾病进展的病理方面。因此,迫切需要开发新的药物,不仅要解决疾病的基本机制,还要表现出神经保护特性。全球的各个研究小组都在使用不同的核心支架设计来开发用于 AD 改善的多功能药物,其中包括氨基甲酸酯。利斯的明是第一个用于 AD 管理的氨基甲酸酯类药物。氨基甲酸酯片段是利斯的明的核心支架,可作为乙酰胆碱酯酶的潜在抑制剂。在这篇综述中,我们总结了过去 10 年对不同取代基的氨基甲酸酯进行修饰的研究,这些取代基主要针对 ChE 抑制、降低氧化应激和调节 Aβ 聚集。